Yuan Sheng-qun
2007
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Journal
Chinese Journal of Bioprocess Engineering
Abstract
The balofloxacin,an new antibacterial agent,was synthesized.The key intermediate 3-methylaminopiperidine was synthesized from 3-bromopyridine with catalyst via ammonolysis and hydrogenization.The effect of hydrogenation using various of catalyst and reaction temperature were studied.Then the balofloxacin was prepared from ethyl-1-cyclopropyl-6,7-di-fluoro-1,4-dihydro-8-methoxy-4oxoquinoline-3-carboxylate via boron chelating in acetic anhydride followed by condensation with the 3-methylaminopiperdine and hydrolysis.The total mass yield of balofloxacin was 58.8%,and the mass yield of 3-methylaminopyridine was 74.1%.The synthetic method was improved by using acetontrile as condensation solvent and as basic reagent.The yield of hydrogenation for synthesizing 3-methylaminopiperidine was 78% with choosing Rh/C as catalyst and the optimal reaction temperature was 80 ℃.